Volasertib (trihydrochloride)

Volasertib (BI 6727) trihydrochloride is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib trihydrochloride inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib trihydrochloride induces mitotic arrest and apoptosis. Volasertib trihydrochloride, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models[1][2].

Product Specifications

CAS Number

[946161-17-7]

Product Name Alternative

BI 6727 (trihydrochloride)

UNSPSC

12352005

Target

Apoptosis; Polo-like Kinase (PLK)

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/volasertib-trihydrochloride.html

Purity

99.12

Solubility

H2O : ≥ 100 mg/mL

Smiles

O=C(C1=CC=C(C(OC)=C1)NC2=NC=C(N(C3=O)C)C(N([C@@H]3CC)C(C)C)=N2)N[C@H]4CC[C@@H](CC4)N5CCN(CC5)CC6CC6.[H]Cl.[H]Cl.[H]Cl

Molecular Formula

C34H53Cl3N8O3

Molecular Weight

728.20

References & Citations

[1]Xie FF, et al. Volasertib suppresses tumor growth in cervical cancer. Am J Cancer Res. 2015 Nov 15;5 (12) :3548-59.|[2]Rudolph D, et al. BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity.Clin Cancer Res. 2009 May 1;15 (9) :3094-102. Epub